[CAS NO. 12772-57-5] Radicicol
PRODUCTS SPECIFICATIONS [12772-57-5]
DESCRIPTION [12772-57-5]
Overview
| MDL | MFCD06795865 |
|---|---|
| Molecular Weight | 364.78 |
| Molecular Formula | C18H17ClO6 |
| SMILES | OC1=C2C(CC(/C=C/C=C\[C@@H](O3)[C@H]3C[C@@H](C)OC2=O)=O)=C(Cl)C(O)=C1 |
1 Publications Citing Use of MCE
Summary
Radicicol is an inhibitor of Hsp90 with an IC 50 value < 1 μM, and leads to proteasomal degradation [1] . Radicicol exhibits inhibition on PDK with IC 50 s of 230 μM ( PDK1 ) and 400 μM ( PDK3 ). Radicicol is an antifungal and antimalarial antibiotic , impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB [2] . Radicicol is also an inhibitor of fat mass and obesity-associated protein ( FTO ), with an IC 50 value of 16.04 μM [3] .
IC50 & Target
|
HSP90 1 μM (IC 50 ) |
Plasmodium
|
In Vitro
Radicicol (1 μM or 100 μM) inhibits the activities of Hsp90 and Topo VI by blocking ATP binding
[1]
.
Radicicol (100 μM; 10 min) binds to ATP-binding site in the C-terminal domain of PDK3 and prevents maturation of
Hsp90
clients
[1]
.
Radicicol (0.25-18 μM; 48 h) inhibits
P. falciparum
3D7 growth with an IC
50
value of 8.563 μM, and (8 μM; 50 h) delays the schizont-to-ring transition
[2]
.
Radicicol (1.5 μM; 40 h) suppresses mitochondrial DNA replication without affecting nuclear and apicoplast genomes
[2]
.
Radicicol (0.001-5 μM; 72 h) induces myoblast differentiation with the myoblast toxicity concentration of 0.1 μM
[5]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [2]
| Cell Line: | P. falciparum 3D7 |
| Concentration: | 0.25 μM, 0.75 μM, 2 μM, 4 μM, 6 μM, 8 μM, 10 μM, 14 μM, 17 μM |
| Incubation Time: | 48 hours |
| Result: | Showed a dose-dependent inhibitory effect on parasite growth. |
Cell Cytotoxicity Assay [5]
| Cell Line: | Primary myoblasts (from mice hindlimb muscles) |
| Concentration: | 0.001, 0.01, 0.1, 1, 5 μM |
| Incubation Time: | 72 hours |
| Result: | Induced myoblast differentiation with a highest concentration of not inducing myoblast toxicity of 0.1 μM. |
In Vivo
Radicicol (20 mg/kg or 60 mg/kg; i.p.; twice dosages; 1 h before and after) has renoprotection effect, and ameliorates renal ischemia reperfusion (I/R) injury and increases renal HSP70 mRNA and protein in renal injury mice
[4]
.
Radicicol (0.05 mg/20 g; s.c.; single dose) enhances the regeneration of skeletal muscle injured by crotoxin via decrease of NF-kB activation
[5]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Renal I/R injury model in mice [4] |
| Dosage: | 20 mg/kg or 60 mg/kg |
| Administration: | Intraperitoneal injection; twice dosages; 1 h before and just after bilateral renal ischemia reperfusion (I/R) |
| Result: | Showed renoprotection effect by inducing renal HSP70 expressing. |
| Animal Model: | Male C57B1/6 mice (3-month-old, 25±2 g) [5] |
| Dosage: | 0.05 mg/20 g |
| Administration: | Subcutaneous injection; single dose; immediately before CTX injury (~1 min); evaluated on day one or 10 after injection |
| Result: |
Resulted heat shock protein induction and decreased NF-kB activation in muscle injured by crotoxin at days 10.
Improved the size recovery of regenerating myofibers and decreased NF-kB activation. |
Appearance
Solid
Source
Penicillium meleagrinum
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 274.14 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7414 mL | 13.7069 mL | 27.4138 mL |
| 5 mM | 0.5483 mL | 2.7414 mL | 5.4828 mL |
| 10 mM | 0.2741 mL | 1.3707 mL | 2.7414 mL |
References
- [1] Kato M, et al. Distinct structural mechanisms for inhibition of pyruvate dehydrogenase kinase isoforms by AZD7545, dichloroacetate, and radicicol. Structure. 2007 Aug;15(8):992-1004. Epub 2007 Aug 2.
- [2] Chalapareddy S, et al. Radicicol confers mid-schizont arrest by inhibiting mitochondrial replication in Plasmodium falciparum. Antimicrob Agents Chemother. 2014 Aug;58(8):4341-52.
- [3] Wang R, et al. Identification of Natural Compound Radicicol as a Potent FTO Inhibitor. Mol Pharm. 2018 Sep 4;15(9):4092-4098.
- [4] Sonoda H, et al. The protective effect of radicicol against renal ischemia--reperfusion injury in mice. J Pharmacol Sci. 2010;112(2):242-6.
- [5] Nascimento TL, et al. Radicicol enhances the regeneration of skeletal muscle injured by crotoxin via decrease of NF-kB activation. Toxicon. 2019 Sep;167:6-9.
Synonyms